Synthesis of unlabelled, 3H- and 125I-labelled β-CIT and its ϖ-fluoroalkyl analogues β-CIT-FE and β-CIT-FP, including synthesis of precursors

The full synthesis of the cocaine congener 2β‐carbomethoxy‐3β‐(4‐iodophenyl)tropane (β‐CIT) and its N‐fluoroalkyl analogues, fluoroethyl‐ and fluoropropyl‐nor‐β‐CIT (β‐CIT‐FE and β‐CIT‐FP) starting from cocaine is described. The synthetic routes include the preparation of precursors for labelling wi...

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Published inJournal of labelled compounds & radiopharmaceuticals Vol. 38; no. 7; pp. 675 - 685
Main Authors Swahn, Carl-Gunnar, Halldin, Christer, Günther, Ilonka, Patt, Jörg, Ametamey, Simon
Format Journal Article
LanguageEnglish
Published Chichester John Wiley & Sons, Ltd 01.07.1996
Subjects
125I
dopamine transporter
β-CIT
β-CIT-FE
β-CIT-FP
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Summary:The full synthesis of the cocaine congener 2β‐carbomethoxy‐3β‐(4‐iodophenyl)tropane (β‐CIT) and its N‐fluoroalkyl analogues, fluoroethyl‐ and fluoropropyl‐nor‐β‐CIT (β‐CIT‐FE and β‐CIT‐FP) starting from cocaine is described. The synthetic routes include the preparation of precursors for labelling with radionuclides such as 11C, 18F, 76Br, 123I, 125I and 3H. Here we also report the labelling with 125I or 3H for use in autoradiographic examination of human brain sections.
Bibliography:Swedish Medical Research Council - No. 03560, 09114
Kasolinska Institutet
istex:560A460195F89E5418A9341E17BE115340E1A1D1
ark:/67375/WNG-D0CTRV1B-3
Swedish Natural Research Council - No. K-KU 9973-307
ArticleID:JLCR880
ISSN:0362-4803
1099-1344
DOI:10.1002/(SICI)1099-1344(199607)38:7<675::AID-JLCR880>3.0.CO;2-L